Purpose: The purpose of this study was to record the utilization of medicinal plants by the Oromo people in the Kofale District, Oromia Regional State, Ethiopia, to control human and animal health problems.
Methods: Data regarding the use of medicinal plants were collected using ethnobotanical methods from 84 traditional medicine practitioners and 304 general informants sampled employing purposive and systematic random sampling methods, respectively, in the Kofale District. Data were analyzed using different indices, including a preference ranking exercise, informant consensus factor (ICF), fidelity level (FL) and relative popularity level (RPL).
Results: In the district, 106 medicinal plants were claimed to be used for the treatment of 43 human and 18 livestock illnesses, of which 75 (71%) were used to manage human health problems, 23 (21.5%) were used to treat both human and livestock ailments and eight (7.5%) were utilized to treat manage livestock health problems. Most (76.4%) plants were harvested from the wild. Leaves were the most commonly used plant part (55.6%) in remedy preparations. Skin diseases scored the highest ICF value (0.97), followed by gastrointestinal disorders (ICF = 0.95), cancer (ICF = 0.93), and hemorrhoids (ICF = 0.91). Medicinal plants that record the highest fidelity level (FL) (100%) and rank order priority (ROP) (100%) values included Justicia schimperiana, Embelia schimperi, Ekebergia capensis and Datura stramonium, which have been used to treat liver disorders, tapeworm infections, babesiosis, and rabies, respectively. There were significant differences (p<0.05) in the mean numbers of medicinal plants claimed by different social groups: older, illiterate, and traditional medicine practitioners reported higher mean numbers of medicinal plants than younger, literate, and general informants, respectively.
Conclusion: This study indicated the richness of medicinal plant species in Kofale District. Medicinal plants with the highest FL and ROP values and those used to treat disease categories with the highest ICF values should be prioritized in future phytochemical and pharmacological investigations.
{"title":"Medicinal Plants Used by Oromo Community in Kofale District, West-Arsi Zone, Oromia Regional State, Ethiopia.","authors":"Geritu Bedasso Nuro, Ketema Tolossa, Mirutse Giday","doi":"10.2147/JEP.S449496","DOIUrl":"10.2147/JEP.S449496","url":null,"abstract":"<p><strong>Purpose: </strong>The purpose of this study was to record the utilization of medicinal plants by the Oromo people in the Kofale District, Oromia Regional State, Ethiopia, to control human and animal health problems.</p><p><strong>Methods: </strong>Data regarding the use of medicinal plants were collected using ethnobotanical methods from 84 traditional medicine practitioners and 304 general informants sampled employing purposive and systematic random sampling methods, respectively, in the Kofale District. Data were analyzed using different indices, including a preference ranking exercise, informant consensus factor (ICF), fidelity level (FL) and relative popularity level (RPL).</p><p><strong>Results: </strong>In the district, 106 medicinal plants were claimed to be used for the treatment of 43 human and 18 livestock illnesses, of which 75 (71%) were used to manage human health problems, 23 (21.5%) were used to treat both human and livestock ailments and eight (7.5%) were utilized to treat manage livestock health problems. Most (76.4%) plants were harvested from the wild. Leaves were the most commonly used plant part (55.6%) in remedy preparations. Skin diseases scored the highest ICF value (0.97), followed by gastrointestinal disorders (ICF = 0.95), cancer (ICF = 0.93), and hemorrhoids (ICF = 0.91). Medicinal plants that record the highest fidelity level (FL) (100%) and rank order priority (ROP) (100%) values included <i>Justicia schimperiana, Embelia schimperi, Ekebergia capensis</i> and <i>Datura stramonium</i>, which have been used to treat liver disorders, tapeworm infections, babesiosis, and rabies, respectively. There were significant differences (<i>p</i><0.05) in the mean numbers of medicinal plants claimed by different social groups: older, illiterate, and traditional medicine practitioners reported higher mean numbers of medicinal plants than younger, literate, and general informants, respectively.</p><p><strong>Conclusion: </strong>This study indicated the richness of medicinal plant species in Kofale District. Medicinal plants with the highest FL and ROP values and those used to treat disease categories with the highest ICF values should be prioritized in future phytochemical and pharmacological investigations.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"16 ","pages":"81-109"},"PeriodicalIF":0.0,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10929209/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140110385","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Background: People frequently complain of long-term constipation. The cost associated with using modern medications to treat constipation is significant, and the probability of encountering side effects is notably high. These limitations restrict their effectiveness in therapy, remain unresolved, and underscore the need for research on alternative therapeutic approaches. Plants of the genus Artemisia have been used to treat constipation. Therefore, the aim of this study was to evaluate the laxative effects of aqueous A. abyssinica leaf and stem extracts of Artemisia abyssinica in mice. Methods: The laxative activity of A. abyssinica leaf and stem extracts was evaluated using three models: laxative activity, gastrointestinal motility, and gastrointestinal secretion. In this study, bisacodyl was used as a standard laxative and loperamide was used to induce constipation. Results: In the laxative test, 200 (P<0.05) and 400 mg/kg (p<0.01) doses of plant extract significantly increased the percentage of fecal water content. Moreover, the highest dose of extract increased the frequency of defecation after 12 h (p<0.05). In the remaining two models, the experimental plans also showed significantly higher gastrointestinal motility and noticeable accumulation of intestinal fluid. Conclusion: The results of this study indicate that aqueous leaf and stem extracts of A. abyssinica have laxative effects.
{"title":"Evaluations of the in vivo Laxative Effects of Aqueous Leaf and Stem Extracts of Artemisia Abyssinica in Mice","authors":"A. Ayele, Jeylan Kawet","doi":"10.2147/jep.s456029","DOIUrl":"https://doi.org/10.2147/jep.s456029","url":null,"abstract":"Background: People frequently complain of long-term constipation. The cost associated with using modern medications to treat constipation is significant, and the probability of encountering side effects is notably high. These limitations restrict their effectiveness in therapy, remain unresolved, and underscore the need for research on alternative therapeutic approaches. Plants of the genus Artemisia have been used to treat constipation. Therefore, the aim of this study was to evaluate the laxative effects of aqueous A. abyssinica leaf and stem extracts of Artemisia abyssinica in mice. Methods: The laxative activity of A. abyssinica leaf and stem extracts was evaluated using three models: laxative activity, gastrointestinal motility, and gastrointestinal secretion. In this study, bisacodyl was used as a standard laxative and loperamide was used to induce constipation. Results: In the laxative test, 200 (P<0.05) and 400 mg/kg (p<0.01) doses of plant extract significantly increased the percentage of fecal water content. Moreover, the highest dose of extract increased the frequency of defecation after 12 h (p<0.05). In the remaining two models, the experimental plans also showed significantly higher gastrointestinal motility and noticeable accumulation of intestinal fluid. Conclusion: The results of this study indicate that aqueous leaf and stem extracts of A. abyssinica have laxative effects.","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"515 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140281763","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Metages Akinaw, Suresh P Nair, Rashed Usure, Bati Leta, Abdo Kedir, Selam Mola, N. Waritu, Mohammed Jemal, Berhane Mulat
Background: Drug-induced kidney injury was among the most common renal damages, from which gentamicin occupies around 25% of this injury. Gentamicin-induced renal damage is caused by increased free radicals with subsequent amplified inflammation. Ajuga remota leaf extract has many phytochemicals with antioxidant activities, which may improve gentamicin-induced renal damage. Thus, we aimed to investigate the nephroprotective effect of Ajuga remota leaf methanolic extract on gentamicin-induced nephrotoxicity in Swiss Albino Mice. Methods: An experimental study design was used on 30 experimental mice randomly allocated in six groups: Group I, II, II, IV, and VI, among which mice were given only distilled water, only gentamicin, 600 mg/kg Ajuga remota leaf extract only, gentamicin along with 200 mg/kg extract, gentamicin with 400 mg/kg extract and gentamicin with 600 mg/kg extract, respectively. At the end of the experiment, the mice were sacrificed after being anaesthetized, and blood samples were collected through a cardiac puncture for renal function tests while the kidneys were removed for histopathological evaluation. The data were entered into Epidata version 4.6 and exported to SPSS version 25 for further analysis using one-way analysis of variance. Statistical significance was set at p < 0.05. Results: Group II mice had significantly higher levels of serum creatinine and blood urea levels compared to group I and III. The body weight of the mice in group V and group VI showed a significant increase compared with Group II. Serum creatinine and blood urea levels were reduced significantly in the Ajuga remota leaf extract administered group of mice compared to group II. Abnormal kidney architectural changes were seen among group II mice; however, those changes were improved after administration of Ajuga remota leaf methanolic extract. Conclusion: Methanol extract of Ajuga remota leaf provided effective protection against gentamicin-induced oxidative renal damage through its antioxidant effects.
{"title":"Nephroprotective Effect of the Leaf Extract of Ajuga remota Benth Against Gentamicin-Induced Nephrotoxicity in Swiss Albino Mice","authors":"Metages Akinaw, Suresh P Nair, Rashed Usure, Bati Leta, Abdo Kedir, Selam Mola, N. Waritu, Mohammed Jemal, Berhane Mulat","doi":"10.2147/jep.s455226","DOIUrl":"https://doi.org/10.2147/jep.s455226","url":null,"abstract":"Background: Drug-induced kidney injury was among the most common renal damages, from which gentamicin occupies around 25% of this injury. Gentamicin-induced renal damage is caused by increased free radicals with subsequent amplified inflammation. Ajuga remota leaf extract has many phytochemicals with antioxidant activities, which may improve gentamicin-induced renal damage. Thus, we aimed to investigate the nephroprotective effect of Ajuga remota leaf methanolic extract on gentamicin-induced nephrotoxicity in Swiss Albino Mice. Methods: An experimental study design was used on 30 experimental mice randomly allocated in six groups: Group I, II, II, IV, and VI, among which mice were given only distilled water, only gentamicin, 600 mg/kg Ajuga remota leaf extract only, gentamicin along with 200 mg/kg extract, gentamicin with 400 mg/kg extract and gentamicin with 600 mg/kg extract, respectively. At the end of the experiment, the mice were sacrificed after being anaesthetized, and blood samples were collected through a cardiac puncture for renal function tests while the kidneys were removed for histopathological evaluation. The data were entered into Epidata version 4.6 and exported to SPSS version 25 for further analysis using one-way analysis of variance. Statistical significance was set at p < 0.05. Results: Group II mice had significantly higher levels of serum creatinine and blood urea levels compared to group I and III. The body weight of the mice in group V and group VI showed a significant increase compared with Group II. Serum creatinine and blood urea levels were reduced significantly in the Ajuga remota leaf extract administered group of mice compared to group II. Abnormal kidney architectural changes were seen among group II mice; however, those changes were improved after administration of Ajuga remota leaf methanolic extract. Conclusion: Methanol extract of Ajuga remota leaf provided effective protection against gentamicin-induced oxidative renal damage through its antioxidant effects.","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"57 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140403370","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Introduction: The potato (Solanum tuberosum L.) is a short-lived tuber plant with a round to oval shape and varying colors, depending on the variety. It is known that only the inside of the potato is used, while the peel is generally discarded. However, recent studies have shown that potato peels contain many health-beneficial compounds.
Purpose: This study aimed to investigate the compounds present in potato peels and their in vitro activities.
Methods: A scoping review following the PRISMA guidelines was conducted. The selection process involved identifying articles of in vitro research published within the last 10 years (2012-2022). Electronic searches were conducted using the portals Scopus, ScienceDirect, EBSCOhost, and Portal Garuda by using the keywords "potato" or "Solanum tuberosum" and "peel" or "skin". The search was limited to articles in English with full text availability.
Results: The screening process resulted in a total of 4773 articles from the four search engines; 14 articles were obtained that met the requirements for the review, most of which use extract preparations in their research. Extracts of flavonoids, phenols, and glycoalkaloids are the most frequently studied compounds, and their antioxidant and anti-inflammatory activity have undergone extensive research.
Conclusion: The potential compounds contained in potato peels, including flavonoids, phenols, and glycoalkaloids, are highly abundant and offer numerous benefits. Provides opportunities for further research to prove the potential pathway activity of the compound. These compounds have been the subject of extensive research, suggesting their significance in the context of health and nutrition.
{"title":"Pharmacological Activity of Chemical Compounds of Potato Peel Waste (<i>Solanum tuberosum</i> L.) in vitro: A Scoping Review.","authors":"Wahyu Hidayat, Irna Sufiawati, Mieke Hemiawati Satari, Ronny Lesmana, Solachuddin Ichwan","doi":"10.2147/JEP.S435734","DOIUrl":"10.2147/JEP.S435734","url":null,"abstract":"<p><strong>Introduction: </strong>The potato (<i>Solanum tuberosum L</i>.) is a short-lived tuber plant with a round to oval shape and varying colors, depending on the variety. It is known that only the inside of the potato is used, while the peel is generally discarded. However, recent studies have shown that potato peels contain many health-beneficial compounds.</p><p><strong>Purpose: </strong>This study aimed to investigate the compounds present in potato peels and their in vitro activities.</p><p><strong>Methods: </strong>A scoping review following the PRISMA guidelines was conducted. The selection process involved identifying articles of in vitro research published within the last 10 years (2012-2022). Electronic searches were conducted using the portals Scopus, ScienceDirect, EBSCOhost, and Portal Garuda by using the keywords \"potato\" or \"Solanum tuberosum\" and \"peel\" or \"skin\". The search was limited to articles in English with full text availability.</p><p><strong>Results: </strong>The screening process resulted in a total of 4773 articles from the four search engines; 14 articles were obtained that met the requirements for the review, most of which use extract preparations in their research. Extracts of flavonoids, phenols, and glycoalkaloids are the most frequently studied compounds, and their antioxidant and anti-inflammatory activity have undergone extensive research.</p><p><strong>Conclusion: </strong>The potential compounds contained in potato peels, including flavonoids, phenols, and glycoalkaloids, are highly abundant and offer numerous benefits. Provides opportunities for further research to prove the potential pathway activity of the compound. These compounds have been the subject of extensive research, suggesting their significance in the context of health and nutrition.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"16 ","pages":"61-69"},"PeriodicalIF":0.0,"publicationDate":"2024-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10849911/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139706954","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To explore the potential therapeutic effects of Physalis angulata L. (Ciplukan) extract on lung fibrosis resolution in a Bleomycin-induced mouse model, researchers conducted a comprehensive study. The study focused on key genes associated with fibrosis progression, including Nox4, Mmp8, Klf4, and FAS, and assessed their mRNA expression levels following the administration of Ciplukan extract.
Methods: A Bleomycin-induced mice model was divided into seven groups to investigate the effects of ciplukan extract on fibrosis-related gene expressions. Mice were induced with subcutaneously injected Bleomycin to generate lung fibrosis and given different doses of the Ciplukan extract for four weeks. Lung fibrosis mRNA expression was analyzed by semi-quantitative PCR for Nox4, Klf4, Mmp8, and FAS.
Results: The administration of ciplukan extract resulted in a significant decrease in mRNA expression of Nox4 with p-value=0.000, Mmp8 with p-value =0.002, and Klf4 with p-value =0.007, indicating potential antifibrotic effects. However, FAS expression remained unchanged (p-value=0.127).
Conclusion: Ciplukan extract exhibited promising effects on fibrosis-related gene expressions, particularly Nox4, Mmp8, and Klf4. This study suggests that the extract has the potential to intervene in fibrosis progression, offering a potential avenue for therapeutic strategies.
{"title":"The Effect of <i>Physalis angulata L</i>. Administration on Gene Expressions Related to Lung Fibrosis Resolution in Mice-Induced Bleomycin.","authors":"Ummul Khair Imaduddin, Afiat Berbudi, Enny Rohmawaty","doi":"10.2147/JEP.S439932","DOIUrl":"10.2147/JEP.S439932","url":null,"abstract":"<p><strong>Purpose: </strong>To explore the potential therapeutic effects of <i>Physalis angulata L</i>. (Ciplukan) extract on lung fibrosis resolution in a Bleomycin-induced mouse model, researchers conducted a comprehensive study. The study focused on key genes associated with fibrosis progression, including Nox4, Mmp8, Klf4, and FAS, and assessed their mRNA expression levels following the administration of Ciplukan extract.</p><p><strong>Methods: </strong>A Bleomycin-induced mice model was divided into seven groups to investigate the effects of ciplukan extract on fibrosis-related gene expressions. Mice were induced with subcutaneously injected Bleomycin to generate lung fibrosis and given different doses of the Ciplukan extract for four weeks. Lung fibrosis mRNA expression was analyzed by semi-quantitative PCR for Nox4, Klf4, Mmp8, and FAS.</p><p><strong>Results: </strong>The administration of ciplukan extract resulted in a significant decrease in mRNA expression of Nox4 with <i>p</i>-value=0.000, Mmp8 with <i>p</i>-value =0.002, and Klf4 with <i>p</i>-value =0.007, indicating potential antifibrotic effects. However, FAS expression remained unchanged (<i>p</i>-value=0.127).</p><p><strong>Conclusion: </strong>Ciplukan extract exhibited promising effects on fibrosis-related gene expressions, particularly Nox4, Mmp8, and Klf4. This study suggests that the extract has the potential to intervene in fibrosis progression, offering a potential avenue for therapeutic strategies.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"16 ","pages":"49-60"},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10840535/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139692012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To assess the permeability of the test item (a combination of curcumin and piperine) and a reference item (dried and crushed turmeric rhizomes) using a combination of Caco-2 cell monolayer permeability assay and liquid chromatography-tandem mass spectrometry.
Methodology: In the Caco-2 cell assay, a transport buffer was prepared, and stock solutions of test and reference items were made. Caco-2 cells were cultured on transwell plates. Permeability assays were conducted for 2 and 6 hours, followed by post-experiment testing for assessing the monolayer integrity. LC-MS/MS (Liquid Chromatography with tandem mass spectrometry) analysis was performed to calculate apparent permeability of each item.
Results: The test item was undetectable at the end of 2 hours of permeability assay. Further, after 6 hours of permeability assay, the permeability of both test and reference item was found to be low.
Conclusion: The results showed that the curcumin and piperine combination had low permeability of curcumin in vitro as compared to the dried and crushed turmeric rhizomes. This could predict the low bioavailability of curcumin in vivo when co-administered with piperine.
{"title":"Investigating Bioavailability of Curcumin and Piperine Combination in Comparison to Turmeric Rhizomes: An in vitro Study.","authors":"Varalakshmi Lalithya Pratti, Muthumani Thomas, Rachana Bhoite, Vinita Satyavrat","doi":"10.2147/JEP.S427818","DOIUrl":"10.2147/JEP.S427818","url":null,"abstract":"<p><strong>Purpose: </strong>To assess the permeability of the test item (a combination of curcumin and piperine) and a reference item (dried and crushed turmeric rhizomes) using a combination of Caco-2 cell monolayer permeability assay and liquid chromatography-tandem mass spectrometry.</p><p><strong>Methodology: </strong>In the Caco-2 cell assay, a transport buffer was prepared, and stock solutions of test and reference items were made. Caco-2 cells were cultured on transwell plates. Permeability assays were conducted for 2 and 6 hours, followed by post-experiment testing for assessing the monolayer integrity. LC-MS/MS (Liquid Chromatography with tandem mass spectrometry) analysis was performed to calculate apparent permeability of each item.</p><p><strong>Results: </strong>The test item was undetectable at the end of 2 hours of permeability assay. Further, after 6 hours of permeability assay, the permeability of both test and reference item was found to be low.</p><p><strong>Conclusion: </strong>The results showed that the curcumin and piperine combination had low permeability of curcumin in vitro as compared to the dried and crushed turmeric rhizomes. This could predict the low bioavailability of curcumin in vivo when co-administered with piperine.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"16 ","pages":"37-47"},"PeriodicalIF":0.0,"publicationDate":"2024-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10838102/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139681229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-16eCollection Date: 2024-01-01DOI: 10.2147/JEP.S433524
Jennie Garcia-Olivares, Brittney Yegla, Frank P Bymaster, Jami Earnest, Jennifer Koch, Chungping Yu, Jonathan Rubin
Background: Viloxazine ER (viloxazine extended-release capsules; Qelbree®), a nonstimulant attention-deficit/hyperactivity disorder (ADHD) treatment, has known activity as a norepinephrine (NE) transporter (NET) inhibitor. In vitro studies have also shown direct pharmacological effects on specific serotonin (5-HT) receptors, but not on the serotonin transporter (SERT). An in vivo microdialysis study in rats showed viloxazine (50 mg/kg i.p.) increased extracellular 5-HT, NE, and dopamine (DA) in the prefrontal cortex (PFC), a key brain region in ADHD pathology. This study evaluated whether these effects occur at clinically relevant concentrations.
Methods: Microdialysis experiments were conducted in freely-moving, Sprague-Dawley rats (males, 8 weeks). Viloxazine (1, 3, 10, 30 mg/kg) was administered intraperitoneally to establish the dose range in rats at which viloxazine plasma concentrations aligned with those of individuals with ADHD administered therapeutic doses of viloxazine ER. Concentrations of unbound viloxazine, NE, 5-HT, DA, and NE and 5-HT metabolites (3,5-dihydroxyphenylglycol [DHPG] and 5-hydroxyindoleacetic acid [5-HIAA]) were measured in PFC interstitial fluid. After identifying a therapeutically relevant dose (30 mg/kg), the experiment was repeated using 30 and 50 mg/kg viloxazine (as 50 mg/kg increased NE, 5-HT, and DA in prior studies).
Results: Viloxazine unbound (free drug) plasma concentrations in rats at 30 mg/kg were comparable to free drug concentrations in individuals with ADHD taking clinically effective doses (based on validated population PK models). Viloxazine 30 mg/kg significantly increased extracellular NE, 5-HT, and DA PFC levels compared to vehicle. Concomitant decreases in DHPG, but not 5-HIAA, support the inhibitory effect of viloxazine on NET but not SERT.
Conclusion: At clinically relevant concentrations, viloxazine increases PFC NE, DA, and 5-HT. Prefrontal augmentation of 5-HT does not appear to result from 5-HT reuptake inhibition but may be related to activation of 5-HT neurons. The potential therapeutic role of serotonergic effects in ADHD treatment merits further exploration.
{"title":"Viloxazine Increases Extracellular Concentrations of Norepinephrine, Dopamine, and Serotonin in the Rat Prefrontal Cortex at Doses Relevant for the Treatment of Attention-Deficit/Hyperactivity Disorder.","authors":"Jennie Garcia-Olivares, Brittney Yegla, Frank P Bymaster, Jami Earnest, Jennifer Koch, Chungping Yu, Jonathan Rubin","doi":"10.2147/JEP.S433524","DOIUrl":"10.2147/JEP.S433524","url":null,"abstract":"<p><strong>Background: </strong>Viloxazine ER (viloxazine extended-release capsules; Qelbree<sup>®</sup>), a nonstimulant attention-deficit/hyperactivity disorder (ADHD) treatment, has known activity as a norepinephrine (NE) transporter (NET) inhibitor. In vitro studies have also shown direct pharmacological effects on specific serotonin (5-HT) receptors, but not on the serotonin transporter (SERT). An in vivo microdialysis study in rats showed viloxazine (50 mg/kg i.p.) increased extracellular 5-HT, NE, and dopamine (DA) in the prefrontal cortex (PFC), a key brain region in ADHD pathology. This study evaluated whether these effects occur at clinically relevant concentrations.</p><p><strong>Methods: </strong>Microdialysis experiments were conducted in freely-moving, Sprague-Dawley rats (males, 8 weeks). Viloxazine (1, 3, 10, 30 mg/kg) was administered intraperitoneally to establish the dose range in rats at which viloxazine plasma concentrations aligned with those of individuals with ADHD administered therapeutic doses of viloxazine ER. Concentrations of unbound viloxazine, NE, 5-HT, DA, and NE and 5-HT metabolites (3,5-dihydroxyphenylglycol [DHPG] and 5-hydroxyindoleacetic acid [5-HIAA]) were measured in PFC interstitial fluid. After identifying a therapeutically relevant dose (30 mg/kg), the experiment was repeated using 30 and 50 mg/kg viloxazine (as 50 mg/kg increased NE, 5-HT, and DA in prior studies).</p><p><strong>Results: </strong>Viloxazine unbound (free drug) plasma concentrations in rats at 30 mg/kg were comparable to free drug concentrations in individuals with ADHD taking clinically effective doses (based on validated population PK models). Viloxazine 30 mg/kg significantly increased extracellular NE, 5-HT, and DA PFC levels compared to vehicle. Concomitant decreases in DHPG, but not 5-HIAA, support the inhibitory effect of viloxazine on NET but not SERT.</p><p><strong>Conclusion: </strong>At clinically relevant concentrations, viloxazine increases PFC NE, DA, and 5-HT. Prefrontal augmentation of 5-HT does not appear to result from 5-HT reuptake inhibition but may be related to activation of 5-HT neurons. The potential therapeutic role of serotonergic effects in ADHD treatment merits further exploration.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"16 ","pages":"13-24"},"PeriodicalIF":0.0,"publicationDate":"2024-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10799649/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139512648","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Eliah Kwizera, Kenneth Ssekatawa, Patrick Aja, Conrad Miruka, Allan Wandera, J. Mpumbya, Robert Siida, Dayyabu Shehu, Tijjani Salihu
{"title":"Methanol Crude Peel Extract of P. granatum Prevents Oxidative Damage in Kidneys of Rats Exposed to Highly Active Antiretroviral Therapy","authors":"Eliah Kwizera, Kenneth Ssekatawa, Patrick Aja, Conrad Miruka, Allan Wandera, J. Mpumbya, Robert Siida, Dayyabu Shehu, Tijjani Salihu","doi":"10.2147/jep.s438368","DOIUrl":"https://doi.org/10.2147/jep.s438368","url":null,"abstract":"","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":" 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139392543","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Putri Anggreini, Hadi Kuncoro, S. Sumiwi, J. Levita
{"title":"Molecular Docking Study of Phytosterols in Lygodium microphyllum Towards SIRT1 and AMPK, the in vitro Brine Shrimp Toxicity Test, and the Phenols and Sterols Levels in the Extract","authors":"Putri Anggreini, Hadi Kuncoro, S. Sumiwi, J. Levita","doi":"10.2147/jep.s438435","DOIUrl":"https://doi.org/10.2147/jep.s438435","url":null,"abstract":"","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"82 11","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139017336","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-24eCollection Date: 2023-01-01DOI: 10.2147/JEP.S437707
Banchayehu Firehun, Teshome Nedi
Background: An ethnobotanical study showed that the leaf of Stephania abyssinica (S. abyssinica) is used for the treatment of gastritis, but there is no scientific investigation.
Objective: The aim of this study was to evaluate the gastroprotective activities of both aqueous and 80% methanol leaf extracts of S. abyssinica in experimental rats.
Methods: Decoction and maceration techniques were used to prepare aqueous and 80% methanol leaf extracts, respectively. The extracts were evaluated against pyloric ligation, indomethacin, and ethanol-induced gastric ulcer models at doses of 100, 200, and 400 mg/kg. Negative control received 2% tween 80, while positive controls received 20 mg/kg of omeprazole and 100 µg/kg of misoprostol. Parameters, such as ulcer index, gastric mucin content, gastric juice volume, pH, and free and total acidity were measured.
Results: In the pyloric ligation induced gastric ulcer model, all doses of both extracts significantly reduced the ulcer index and gastric juice volume, while doses of 200 and 400 mg/kg exhibited a significant increment in mucus content and gastric juice pH as well as decrease in free and total acidity as compared to negative control. In indomethacin and ethanol induced gastric ulcer models, pretreatment with both extracts significantly reduced the ulcer index and enhanced gastric mucin content in a dose-dependent manner. Phytochemical screening of both extracts showed the existence of flavonoids, phenols, tannins, saponins, alkaloids, and coumarins with high contents of phenols, flavonoids, and alkaloids in 80% methanol extract.
Conclusion: This study revealed that aqueous and 80% methanol leaf extracts of S. abyssinica possessed remarkable gastroprotective activities against experimentally induced gastric ulcer models, and this possibly justify the traditional use of S. abyssinica leaves to treat gastritis.
{"title":"Gastroprotective Activities of Aqueous and 80% Methanol Leaf Extracts of <i>Stephania abyssinica</i> (Quart.-Dill. and A. Rich.) Walp. (Menispermaceae) in Rats.","authors":"Banchayehu Firehun, Teshome Nedi","doi":"10.2147/JEP.S437707","DOIUrl":"10.2147/JEP.S437707","url":null,"abstract":"<p><strong>Background: </strong>An ethnobotanical study showed that the leaf of <i>Stephania abyssinica</i> (<i>S. abyssinica</i>) is used for the treatment of gastritis, but there is no scientific investigation.</p><p><strong>Objective: </strong>The aim of this study was to evaluate the gastroprotective activities of both aqueous and 80% methanol leaf extracts of <i>S. abyssinica</i> in experimental rats.</p><p><strong>Methods: </strong>Decoction and maceration techniques were used to prepare aqueous and 80% methanol leaf extracts, respectively. The extracts were evaluated against pyloric ligation, indomethacin, and ethanol-induced gastric ulcer models at doses of 100, 200, and 400 mg/kg. Negative control received 2% tween 80, while positive controls received 20 mg/kg of omeprazole and 100 µg/kg of misoprostol. Parameters, such as ulcer index, gastric mucin content, gastric juice volume, pH, and free and total acidity were measured.</p><p><strong>Results: </strong>In the pyloric ligation induced gastric ulcer model, all doses of both extracts significantly reduced the ulcer index and gastric juice volume, while doses of 200 and 400 mg/kg exhibited a significant increment in mucus content and gastric juice pH as well as decrease in free and total acidity as compared to negative control. In indomethacin and ethanol induced gastric ulcer models, pretreatment with both extracts significantly reduced the ulcer index and enhanced gastric mucin content in a dose-dependent manner. Phytochemical screening of both extracts showed the existence of flavonoids, phenols, tannins, saponins, alkaloids, and coumarins with high contents of phenols, flavonoids, and alkaloids in 80% methanol extract.</p><p><strong>Conclusion: </strong>This study revealed that aqueous and 80% methanol leaf extracts of <i>S. abyssinica</i> possessed remarkable gastroprotective activities against experimentally induced gastric ulcer models, and this possibly justify the traditional use of <i>S. abyssinica</i> leaves to treat gastritis.</p>","PeriodicalId":15846,"journal":{"name":"Journal of Experimental Pharmacology","volume":"15 ","pages":"497-512"},"PeriodicalIF":0.0,"publicationDate":"2023-11-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10683649/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138460229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}